4-(5-Fluoropyridin-2-yl)-2azetidinones to Fight Against Drug-Resistant Pancreatic Cancer

The University of Texas Rio Grande Valley Background
Around 95% of pancreatic tumors are driven by mutations in KRAS gene, subbed “undruggable” and prevalent in 5 drug-resistant pancreatic cancers. Currently, there is no effective medicine in the market for drug-resistant cancers.
Technology Overview
The present technology consists of compounds that demonstrate outstanding results against drug-resistant cancer cell lines.
6 potent anti-pancreatic cancer 2-azetidinone molecules against drug-resistant cell lines were designed, validated in silico, synthesized through multi-step process, and conducted in vitro anti-pancreatic cancer evaluation (2D-culture & 3D-tumorsphere formation assays). The series consists of 12 small molecules ().
Stage of Development
A prototype is near commercial grade, and has been tested in an operational lab environment.

3 to 359 times more selective towards PANC-1 cells compared to normal pancreatic ductal epithelial cells
Potential antibacterial and drug-resistant antibacterial activity against various types of infections

Value Proposition
These derivatives of compounds show excellent cytotoxicity against drug-resistant pancreatic cancer cell lines (PANC-1 cells): Best IC50 values in 2D-culture and 3D-tumorsphere assays are 2.55 nM and 2.33 nM, respectively.

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